Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.

Article Details

Citation

Copy to clipboard

Nazare M, Essrich M, Will DW, Matter H, Ritter K, Urmann M, Bauer A, Schreuder H, Dudda A, Czech J, Lorenz M, Laux V, Wehner V

Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4191-5.

PubMed ID

15261268 [ View in PubMed

]

Abstract

A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for neutral ligands, which bind in the S1 pocket of factor Xa were investigated with the 2-carboxyindole scaffold. This privileged fragment assembly approach yielded a set of equipotent, selective inhibitors with structurally diverse neutral P1 substituents.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1-{2-[(4-CHLOROPHENYL)AMINO]-2-OXOETHYL}-N-(1-ISOPROPYLPIPERIDIN-4-YL)-1H-INDOLE-2-CARBOXAMIDE	Coagulation factor X	Ki (nM)	3	7.8	25	Details
N-(1-ISOPROPYLPIPERIDIN-4-YL)-1-(3-METHOXYBENZYL)-1H-INDOLE-2-CARBOXAMIDE	Coagulation factor X	Ki (nM)	89	7.8	25	Details